Tenilsetam (CAS 997: ( /-)-3-(2-thienyl)-2-piperazinone), a cognition-enhancing drug successfully used for the treatment of patients suffering from Alzheimer's disease. According to the mechanism proposed, it inhibits advanced glycation end-product (AGE) formation. The beneficial effect of tenilsetam in Alzheimer's disease could come from the interference with AGE-derived crosslinking of amyloid plaques and a decreased inflammatory response to diminished activation of phagocytosing microglia. In addition was shown, that the long-term treatment with tenilsetam inhibited the formation of acellular capillaries without correcting pericyte loss. Was suggested that tenilsetam could be useful for the treatment of early diabetic retinopathy, but then these studies were discontinued.

Terbufibrol, an antihyperlipoproteinemic agent that blocks the hepatic cholesterol synthesis in a step between acetate and HMG-CoA (3-hydroxy-3-methylglutaryl-CoA). Information about the current use of this compound is not available.

Terdecamycin, an antibiotic that was studied on the pigs to treat dysentery. Information about the current use of this drug is not available.

Terbuprol was developed as a choleretic agent that has never been marketed. Information about the current use of this drug is not available.

Terfluranol is a bibenzyl derivative patented by Biorex Laboratories Ltd. as an antineoplastic agent.

Nifluridide, an experimental insecticide, is used for the control of sucking and biting insects such as Phthiraptera. Nifluridide was systemically active against Triatoma infestans on mice and Rhodnius prolixus on cattle.

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta, FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agent exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis. In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy thus supporting the rationale for cancer therapy by induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition. R1530 strongly inhibited human tumor cell proliferation and growth factor-driven proliferation of endothelial and fibroblast cells. Significant tumor growth inhibition was demonstrated in a lung cancer xenograft model with a range of once daily, weekly and twice-weekly doses of R1530. Daily doses were most effective in the lung cancer model and also had significant growth inhibitory effects in models of colorectal, prostate, and breast tumors. Tumor regression occurred in all models treated with the maximum tolerated daily dose. The doses of 25 and 50 mg/kg QD resulted in biologically significant increased survival in all tested models. After oral administration in nude mice, R1530 showed good tissue penetration. R1530 had been in phase I clinical trials by Hoffmann-La Roche, Inc. for the treatment of advanced solid tumors. However, the clinical development of R1530 was discontinued.

3,5-Diiodothyropropionic acid (DITPA), a carboxylic acid analog with low metabolic activity, was observed to induce alpha-MHC mRNA in heart cell culture with EC50 approximately 5 x 10(-7) M. Zarion Pharmaceuticals was developing DITPA (3,5-diiodothyropropionic acid), a thyroid hormone analogue, for the treatment of Allan-Herndon-Dudley syndrome. In May 2013, the US FDA granted DITPA orphan drug status for the treatment of Allan-Herndon-Dudley syndrome. However, development of DITPA for the treatment of Allan-Herndon-Dudley syndrome was discontinued.

Indeglitazar is orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma patented by Plexxikon, Inc for metabolic disorders treatment. Indeglitazar is a full agonist of PPAR alpha but only a partial agonist of PPAR gamma and delta; this may provide a better side effect profile than full activators. The molecule shows impressive pharmaceutical properties (high oral bioavailability, the long half-life, etc.) as well as promising activity in mouse and rat models of diabetes (lower blood glucose, insulin, total cholesterol, triglycerides, free fatty acids, etc.). In contrast to other PPAR agonists, which sometimes cause weight gain, Indeglitazar also caused weight loss in rodent and primate models. Although Indeglitazar was advanced to phase 2 trials in collaboration with Wyeth, increasing concerns over the potential side effects of PPAR agonists have caused Wyeth to discontinue development of this compound

FILAMINAST is a phosphodiesterase 4 inhibitor with bronchorelaxant activity and selectivity of potential use in the treatment of asthma. However, its clinical development was discontinued due to lack of efficacy.